Lysteda (tranexamic acid oral) dosing, indications, interactions, adverse effects, and more

Sections

Sections tranexamic acid oral
Dosing & Uses
Interactions
Adverse Effects
Warnings
Pregnancy
Pharmacology
Images
Patient Handout
Formulary

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

650mg

Menorrhagia

Indicated for the treatment of cyclic heavy menstrual bleeding

1300 mg PO TID for up to 5 days during menstruation

Renal impairment

SCr >1.4 mg/dL and ≤2.8 mg/dL: 1300 mg PO BID
SCr >2.8 mg/dL and ≤5.7 mg/dL: 1300 mg PO qDay
SCr >5.7 mg/dL: 650 mg PO qDay
Each regimen listed above may be administered for up to 5 days during menstruation

Hepatic impairment

Dose adjustments not necessary

Hereditary Angioedema (Off-label)

Long term prophylaxis: 1000-1500 mg PO q8-12hr; reduce dose to 500 mg/dose PO qDay or q12hr when frequency of attacks reduces

Short term prophylaxis: 75 mg/kg/day PO divided q8-12hr for 5 days before and after the event

Treatment of acute HAE attack: 25 mg/kg/dose PO/IV; not to exceed 1000 mg/dose q3-4hr; not to exceed 75 mg/kg/day or 1000 mg PO q6hr for 48 hr

Cone Biopsy (Off-label)

1000-1500 mg q8-12hr x12 days postop

Epistaxis (Off-label)

1000-1500 mg q8-12hr x10 days

Hyphema (Off-label)

1000-1500 mg q8-12hr x7 days

Hereditary Angioedema (Off-label)

1000-1500 mg PO BID/TID

Administration

May take with or without food

Swallow whole, do not chew, break, or crush

Indicated for women of reproductive age and is not intended for use in premenarcheal girls

Based on a pharmacokinetic study in 20 adolescent females, aged 12-16 years, no dose adjustment is needed in the adolescent population

Interaction Checker

Enter a drug name and tranexamic acid oral

No Results

No Interactions Found

Interactions Found

Contraindicated

Serious - Use Alternative

Significant - Monitor Closely

Minor

All Interactions Sort By:

Contraindicated (3)

dienogest/estradiol valerate
tranexamic acid oral, dienogest/estradiol valerate. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
ethinylestradiol
tranexamic acid oral, ethinylestradiol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
mestranol
tranexamic acid oral, mestranol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk .

Serious - Use Alternative (4)

anti-inhibitor coagulant complex
tranexamic acid oral, anti-inhibitor coagulant complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

anti-inhibitor coagulant complex, tranexamic acid oral. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration ma.
Factor IX
tranexamic acid oral, Factor IX. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
Factor IX complex
tranexamic acid oral, Factor IX complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
Factor IX, recombinant
tranexamic acid oral, Factor IX, recombinant. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

Monitor Closely (5)

alteplase
tranexamic acid oral, alteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
defibrotide
tranexamic acid oral decreases effects of defibrotide by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Defibrotide may diminish effects of thrombolytic agents. Consider therapy modification.
reteplase
tranexamic acid oral, reteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
tenecteplase
tranexamic acid oral, tenecteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
tretinoin
tranexamic acid oral, tretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration may increase procoagulant effect.

Minor (0)

alteplase
Monitor Closely (1)tranexamic acid oral, alteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
anti-inhibitor coagulant complex
Serious - Use Alternative (2)tranexamic acid oral, anti-inhibitor coagulant complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

anti-inhibitor coagulant complex, tranexamic acid oral. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration ma.
defibrotide
Monitor Closely (1)tranexamic acid oral decreases effects of defibrotide by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Defibrotide may diminish effects of thrombolytic agents. Consider therapy modification.
dienogest/estradiol valerate
Contraindicated (1)tranexamic acid oral, dienogest/estradiol valerate. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
ethinylestradiol
Contraindicated (1)tranexamic acid oral, ethinylestradiol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
Factor IX
Serious - Use Alternative (1)tranexamic acid oral, Factor IX. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
Factor IX complex
Serious - Use Alternative (1)tranexamic acid oral, Factor IX complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
Factor IX, recombinant
Serious - Use Alternative (1)tranexamic acid oral, Factor IX, recombinant. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
mestranol
Contraindicated (1)tranexamic acid oral, mestranol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk .
reteplase
Monitor Closely (1)tranexamic acid oral, reteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
tenecteplase
Monitor Closely (1)tranexamic acid oral, tenecteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
tretinoin
Monitor Closely (1)tranexamic acid oral, tretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration may increase procoagulant effect.

>10%

Headache (50.4%)

Nasal and sinus symptoms (25.4%)

Back pain (20.7%)

Abdominal pain (19.8%)

Musculoskeletal pain (11.2%)

1-10%

Arthralgia (6.9%)

Muscle cramps and spasms (5.8%)

Migraine (6%)

Anemia (5.6%)

Fatigue (5.2%)

Postmarketing Reports

Nausea, vomiting, and diarrhea

Allergic skin reactions

Anaphylactic shock and anaphylactoid reactions

Thromboembolic events (eg, DVT, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction); cases have been associated with concomitant use of combination hormonal contraceptives Impaired color vision and other visual disturbances

Dizziness

Contraindications

Hypersensitivity

Women using combination hormonal contraceptives

Active thromboembolic disease (eg, DVT, pulmonary embolism, or cerebral thrombosis)

History of thrombosis or thromboembolism, including retinal vein or artery occlusion

Intrinsic risk of thrombosis or thromboembolism (eg, thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy)

Cautions

Increased risk for thrombosis when coadministered with combination oral contraceptive (see Contraindications), Factor IX complex concentrates, anti-inhibitor coagulant concentrates, or oral tretinoin

Venous and arterial thrombosis or thromboembolism, as well as cases of retinal artery and retinal vein occlusions, have been reported

Severe allergic reaction reported; anaphylactic shock reported with IV product

May cause cerebral edema and cerebral infarction in women with subarachnoid hemorrhage

Ligneous conjunctivitis reported

Pregnancy

Not indicated for use in pregnant women; there are no available data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; tranexamic acid crosses the placenta; animal reproduction studies have not identified adverse developmental outcomes with oral administration of tranexamic acid to pregnant rats at doses up to 4 times the recommended human dose

Lactation

Tranexamic acid is present in the mother’s milk at a concentration of about one hundredth of the corresponding serum concentration; the amount of tranexamic acid a nursing infant would absorb is unknown; there are no adequate data on effects of tranexamic acid on breastfed infant or on milk production; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breast-fed child from therapy or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Antifibrinolytic; synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure

Absorption

Bioavailability: 45%

Peak plasma time: 2.5 hr

Peak plasma concentration: 16.41 mcg/mL (steady-state)

AUC: 80.19 mcg•hr/mL

Distribution

Protein bound: 3%

Vd: 0.18 L/kg (initial); 0.39 L/kg (steady-state)

Metabolism

Small fraction is metabolized

Elimination

Half-life: 11.08 hr

Eliminated by urinary excretion primarily via glomerular filtration

Excretion: 90% urine; >95% of the dose excreted unchanged

Images

No images available for this drug.

Patient Handout

A Patient Handout is not currently available for this monograph.

Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Create Your List of Plans

Adding plans allows you to:

View the formulary and any restrictions for each plan.
Manage and view all your plans together – even plans in different states.
Compare formulary status to other drugs in the same class.
Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

View explanations for tiers and restrictions

Tier	Description
1	This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2	This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6	This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC	NOT COVERED – Drugs that are not covered by the plan.

Code	Definition
PA	Prior Authorization Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL	Quantity Limits Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST	Step Therapy Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR	Other Restrictions Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.

Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.

[CLOSE WINDOW]